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US4657899A Expired / Lapsed US ⏱️ 0.0 years remaining

Antagonists of specific excitatory amino acid neurotransmitter receptors

Assignee: Eisai Corp of North America
•
Filing: 1986-04-09
•
Granted: 1987-04-14
•
Expires: 2006-04-09
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Abstract

Abstract The invention pertains to novel, potent anticonvulsants, analgesics and cognition enhancers achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to ω-[2-phosphonoalkyleneyl)phenyl]-2-aminoalkanoic acids having general formula: ##STR1## Wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, --CH═CH--CH═CH═, amino, nitro, trifluoromethyl or cyano; n and m=0, 1, 2, or 3; and the pharmaceutically acceptable salts and derivatives thereof. Examples of specific preferred compounds of general formula are selected from the group consisting of: 4-[2-phosphonomethylphenyl]-2-aminobutanoic acid, ethyl 3-[2-(2-diethylphosphonoethyl)phenyl]-2-acetamido-2-carboethoxypropanoate, 3-[2-(2-phosphonomethyl)phenyl]-2-aminopropanoic acid, ethyl 3-[2-(3-bromopropyl)phenyl]-2-acetamido-3-carboethoxypropanoate, ethyl 3-[2-(3-diethylphosphonopropyl)phenyl]-2-acetamido-2-carboethoxypropanoate, ethyl 3-[2-(3-phosphonopropyl)-phenyl]-2-aminopropanoic acid, ethyl 5-[2-(diethylphosphonomethyl)-phenyl]-2-acetamido-2-carboethoxypentanoate, and 5-[2-phosphonomethylphenyl]-2-aminopentanoic acid.

Inventors

  • 👤 Waclaw J. Rzeszotarski
  • 👤 Robert L. Hudkins
  • 👤 Maria E. Guzewska

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-01 10:45
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3882; A; A61; A61P; A61P25/00; A61P25/04; A61P25/08; C07F9/3834

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 65 words
A potent selective excitatory amino acid neutrotransmitter receptor antagonist having the general formula: ##STR6## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, amino, nitro, triflouromethyl or cyano, or taken together are --CH═CH--CH═3 CH--; n an m=0, 1, 2, or 3; and the pharmaceutically acceptable salts and the 2-acetamido-2-carboethoxy esters thereof.
Claim 2
Dependent Claim 65 words
A potent selective excitatory amino acid neutrotransmitter receptor antagonist having the general formula: ##STR6## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, amino, nitro, triflouromethyl or cyano, or taken together are --CH═CH--CH═3 CH--; n an m=0, 1, 2, or 3; and the pharmaceutically acceptable salts and the 2-acetamido-2-carboethoxy esters thereof.
Claim 3
Dependent Claim 27 words
The potent selective excitatory amino acid neurotransmitter receptor antagonist of claim 1 wherein R 1 R 2 =--CH═CH--CH═CH-- and n=1 and m=2 and the 2-acetamido-2-carboethoxy esters thereof.
Claim 4
Dependent Claim 10 words
The compound according to claim 1 that is 4-[2-phosphonomethylphenyl]-2-amino-butanoic acid.
Claim 5
Dependent Claim 10 words
The compound according to claim 1 that is ethyl 3-[2-(2-diethylphosphonoethyl)-phenyl]-2-acetamido-2-carbethoxypropanoate.
Claim 6
Dependent Claim 10 words
The compound according to claim 1 that is 3-[2-(2-phosphonoethyl)-phenyl]-2-aminopropanoic acid.
Claim 7
Dependent Claim 10 words
The compound according to claim 1 that is 3-[2-phosphonomethylphenyl]-2-amino-propanoic acid.
Claim 8
Dependent Claim 10 words
The compound according to claim 1 that is 3-[2-(3-phosphonopropyl)-phenyl]-2-aminopropanoic acid.
Claim 9
Dependent Claim 10 words
The compound according to claim 1 that is 5-[2-phosphonomethylphenyl]-2-amino-pentanoic acid.
Claim 10
Dependent Claim 28 words
A pharmaceutical composition for relieving pain which comprises a pain relieving effective amount of one or more compounds of claim 1 with a pharmaceutically acceptable carrier and/or diluent.
Claim 11
Dependent Claim 33 words
A process of relieving pain in an animal in need thereof which comprises administering said compound of claim 1 parenterally, nasally, orally, rectally or a combination thereof to said animal in need thereof.
Claim 12
Dependent Claim 29 words
A pharmaceutical composition for treatment of convulsions or epilepsy which comprises an effective amount of one or more compounds of claim 1 with a pharmaceutically acceptable carrier and/or diluent.
Claim 13
Dependent Claim 29 words
A process for treating convulsions or epilepsy which comprises administering said compound of claims 1 parenterally, orally, nasally, rectally or a combination thereof to said animal in need thereof.
Claim 14
Dependent Claim 27 words
A pharmaceutical composition of enhancing cognition which comprises a cognition enhancing amount of one or more compounds of claim 1 with a pharmaceutically acceptable carrier and/or diluent.
Claim 15
Dependent Claim 27 words
A process for enhancing cognition which comprises administering said compound of claim 1 parenterally, orally, nasally, rectally or a combination thereof to said animal in need thereof.

References Cited (Backward Citations)

US2915547A Cited
US2966074A Cited
US3754085A Cited
SU431171A1 Cited
US4061697A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-04-13 1990-10-13 1991-04-14 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-04-13 1994-10-13 1995-04-14 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-04-13 1998-10-13 1999-04-14 $7700.00 Window Closed / Lapsed

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